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Archives of pharmacal research : a publication of ... 22건

  1. [국내논문]   A Stereoselective Asymmetric Synthesis of Antibiotic (-)-Fumagillol Using Claisen Rearrangement and Intramolecular Ester Enolate Alkylation as Key Steps  

    Kim Deukjoon (College of Pharmacy, Seoul National University ) , Ahn Soon Kil (New Drug Research Laboratories, Chong Kun Dang Research Institute Cheonan ) , Bae Hoon (Department of Chemistry and Biochemistry, Florida State University ) , Kim Hak Sung (Wonkwang University, College of Pharmacy)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.2 ,pp. 129 - 141 , 2005 , 0253-6269 ,

    초록

    (-)-Fumagillol (1), a hydrolysis product of fumagillin, has been synthesized by several group from commercially available 1,2:5,6-di-O-isopropylidene- ${\alpha}$ -D-allofuranose in a highly stereoselective manner. Chiral centers on C5 and C6 came from D-allofuranose and the asymmetric center on C4 was accomplished by 1,3-chirality transfer using the Claisen rearrangement on a chiral allyl alcohol. Chirality, which is necessary on an epoxide consisting of the spiro-ring system, was diastereoselectively constructed by the well-known reaction, intramolecular ester enolate alkylation (IEEA), which showed that this reaction can be applied to the alpha-alkoxy ester system. The epoxide on the side chain was regioselectively introduced by the difference between the number of substituents on the vinyl groups. This accomplishment proved that IEEA can be a useful tool for the synthesis of complex molecules.

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  2. [국내논문]   Design and Synthesis of Novel Antidiabetic Agents  

    Lee Joon Yeol (College of Pharmacy & Research Institute of Drug Development, Chonnam National University ) , Park Won-Hui (College of Pharmacy & Research Institute of Drug Development, Chonnam National University ) , Cho Min-Kyoung (College of Pharmacy & Research Institute of Drug Development, Chonnam National University ) , Yun Hyun Jin (College of Pharmacy & Research Institute of Drug Development, Chonnam National University ) , Chung Byung-Ho (College of Pharmacy & Research Institute of Drug Development, Chonnam National University ) , Pak Youngmi Kim (Asan Institute for Life Sciences, Department of Internal Medicine, College of Medicine, University of U1san ) , Hahn Hoh-Gyu (Life Science Division, Korea Institute of Science and Technology ) , Cheon Seung Hoon (College of Pharmacy & Research Institute of Drug Development, Chonnam National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.2 ,pp. 142 - 150 , 2005 , 0253-6269 ,

    초록

    The synthesis and structure-activity relationships of a novel series of substituted quercetins that activates peroxisome proliferator-activated receptor gamma ( $PPAR{\gamma}$ ) are reported. The $PPAR{\gamma}$ agonistic activity of the most potent compound in this series is comparable to that of the thiazolidinedione-based antidiabetic drugs currently in clinical use.

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  3. [국내논문]   Diastereoselective Synthesis of Polysubstituted Pyrrolidinone as a Key Intermediate for the Anticancer Agents by Palladium(II)­Catalyzed Carboxylation  

    Choi Dong-Rack (College of Pharmacy, SungKyunKwan University ) , Lee Kee-Young (College of Pharmacy, SungKyunKwan University ) , Chung Yun-Sung (College of Pharmacy, SungKyunKwan University ) , Joo Jae-Eun (College of Pharmacy, SungKyunKwan University ) , Kim Yong-Hyun (College of Pharmacy, SungKyunKwan University ) , Oh Chang-Young (College of Pharmacy, SungKyunKwan University ) , Lee Yiu-Suk (College of Pharmacy, SungKyunKwan University ) , Ham Won-Hun (College of Pharmacy, SungKyunKwan University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.2 ,pp. 151 - 158 , 2005 , 0253-6269 ,

    초록

    Palladium(II)-catalyzed carboxylation of chiral olefins 6a-d has been examined under various conditions. In the weak basic condition ( $K_{2}CO_3$ ), 7a-d were obtained in good yields. Alternatively, in the strong basic condition, pyrrolidinones 8a-d were obtained resulting in excellent yields and with high diastereoselectivity.

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  4. [국내논문]   Inhibition of Calmodulin-Dependent Protein Kinase II by Cyclic and Linear Peptide Alkaloids from Zizyphus Species  

    Han Yong Nam (Natural Products Research Institute, College of Pharmacy, Seoul National University ) , Hwang Keum Hee (Korea Bio-Food and Drug Research Center, Konkuk University ) , Han Byung Hoon (Natural Products Research Institute, Seoul National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.2 ,pp. 159 - 163 , 2005 , 0253-6269 ,

    초록

    The effects of sedative peptide alkaloids from Zizyphus species on calmodulin- dependent protein kinase II were investigated. Protein kinase II activity was assayed on the basis of its ability to activate tryptophan 5-monooxygenase as its substrate in the presence of calmodulin. All thirteen alkaloids tested were stronger inhibitors than chlorpromazine ( $IC_50,\;98{\mu}M$ ) on calmodulin-dependent protein kinase II. Among them, the most potent inhibitor was daechuine S27 ( $IC_{50},\;2.95{\mu}M$ ), which was stronger than pimozide ( $IC_{50},\;15.0{\mu}M$ ).

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  5. [국내논문]   The Inhibition of Diacylglycerol Acyltransferase by Terpenoids from Youngia koidzumiana  

    Dat Nguyen Tien (College of Pharmacy, Chungnam National University ) , Cai Xing Fu (College of Pharmacy, Chungnam National University ) , Rho Mun-Chual (Cardiovascular Research Laboratory, Korea Research Institute of Bioscience and Biotechnology ) , Lee Hyun Sun (Cardiovascular Research Laboratory, Korea Research Institute of Bioscience and Biotechnology ) , Bae KiHwan (College of Pharmacy, Chungnam National University ) , Kim Young Ho (College of Pharmacy, Chungnam National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.2 ,pp. 164 - 168 , 2005 , 0253-6269 ,

    초록

    The EtOAc extract of Youngia koidzumiana significantly inhibited the diacylglycerol acyltransferase (DGAT) from rat liver microsomes. Bioactivity-guided fractionation led to the isolation of nine compounds, the structures of which were established using physicochemical and spectral data. Of the isolated compounds, oleanolic acid (2), methyl ursolate (7) and corosolic aicd (8) inhibited DGAT, with $IC_{50}$ values of 31.7, 26.4, and $44.3{\mu}M$ , respectively. However, sesquit-erpenoids showed only weak inhibitory effects toward DGAT.

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  6. [국내논문]   Inhibitory Activity of Isorhamnetin from Persicaria thunbergii on Farnesyl Protein Transferase   피인용횟수: 6

    Oh Hyun Mi (Korea Research Institute of Bioscience and Biotechnology, KIST ) , Kwon Byoung-Mog (Korea Research Institute of Bioscience and Biotechnology, KIST ) , Baek Nam-In (Graduate School of Biotechnology & Plant Metabolism Research Center, KyungHee University ) , Kim Sung-Hoon (Graduate School of East-West Medical Science, KyungHee University ) , Chung In-Sik (Graduate School of Biotechnology & Plant Metabolism Research Center, KyungHee University ) , Park Mi-Hyun (Erom Life Co. Ltd. ) , Park Hee Wook (College of Pharmacy, Woosuk University ) , Lee Jae Hyeok (College of Pharmacy, Woosuk University ) , Park Hye Won (College of Pharmacy, Woosuk University ) , Kim Eun Jeong (College of Pharmacy, Woosuk University ) , Kim Dae Keun (College of Pharmacy, Woosuk University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.2 ,pp. 169 - 171 , 2005 , 0253-6269 ,

    초록

    The methanolic extract of the aerial parts of Persicaria thunbergii was found to show inhibitory activity on Farnesyl Protein Transferase (FPTase). Bioassay-guided fractionation of the methanolic extract resulted in the isolation of isorhamnetin, as an inhibitor on FPTase. This compound inhibited FPTase activity in a dose-dependent manner, and the $IC_{50}$ value of isorhamnetin was $37.5\;{\mu}M$ .

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    NDSL에서는 해당 원문을 복사서비스하고 있습니다. 아래의 원문복사신청 또는 장바구니담기를 통하여 원문복사서비스 이용이 가능합니다.

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  7. [국내논문]   Butyrylcholinesterase Inhibitory Guaianolides from Amberboa ramosa  

    Khan Sher Bahadar (International Centre for Chemical Sciences, H.E.J. Research Institute of Chemistry, University of Karachi ) , Haq Azhar-ul (International Centre for Chemical Sciences, H.E.J. Research Institute of Chemistry, University of Karachi ) , Perveen Shagufta (International Centre for Chemical Sciences, H.E.J. Research Institute of Chemistry, University of Karachi ) , Afza Nighat (Pharmaceutical Research Centre, PCSIR Labs Complex Karachi ) , Malik Abdul (International Centre for Chemical Sciences, H.E.J. Research Institute of Chemistry, University of Karachi ) , Nawaz Sarfraz Ahmad (International Centre for Chemical Sciences, H.E.J. Research Institute of Chemistry, University of Karachi ) , Shah Muhammad Raza (International Centre for Chemical Sciences, H.E.J. Research Institute of Chemistry, University of Karachi ) , Choudhary Muhammad lqbal (International Centre for Chemical Sciences, H.E.J. Research Institute of Chemistry, University of Karachi)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.2 ,pp. 172 - 176 , 2005 , 0253-6269 ,

    초록

    Phytochemical investigation of the whole plant of Amberboa ramosa led to the isolation of six sesquiterpene lactones which could be identified as $8{\alpha}$ -hydroxy- $11{\beta}$ -methyl- $1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H,\;11{\alpha}H-guai-10(14)$ , 4(15)-dien-6, 12-olide(2), $3{\beta},\;8{\alpha}-dihydroxy-11{\alpha}-methyl-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H,\;11{\beta}H-guai-10(14)$ , 4(15)-dien-6, 12-olide (2), $3{\beta},\;4{\alpha},\;8{\alpha}-trihydroxy-4{\beta}(hydroxymethyl)-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H-guai-10(14)$ , 11(13)-dien-6, 12-olide (3), $3{\beta},\;4{\alpha},\;8{\alpha}-trihydroxy-4{\beta}-(chloromethyl)-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H-guai-10(14)$ , 11(13)-dien-6, 12-olide(4), $3{\beta},\;4{\alpha},\;dihydroxy-4{\beta}-(hydroxymethyl)-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H-guai-10(14)$ , 11(13)-dien-6, 12-olide(5), $3{\beta},\;4{\alpha}-dihydroxy-4{\beta}-(chloromethyl)-8{\alpha}-(4-hydroxymethacrylate)-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H-guai-10(14)$ , 11(13)-dien-6, 12-olide (6) by spectroscopic methods. All of them showed inhibitory potential against butyrylcholinesterase.

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  8. [국내논문]   Nitric Oxide and Prostaglandin $E_2$ Synthesis Inhibitory Activities of Diarylheptanoids from the Barks of Alnus japonica Steudel   피인용횟수: 6

    Kim Hyun-Jung (College of Pharmacy, Chung Ang University ) , Yeom Seung-Hwan (College of Pharmacy, Chung Ang University ) , Kim Min-Kee (College of Pharmacy, Chung Ang University ) , Shim Jae-Geul (College of Pharmacy, Chung Ang University ) , Paek In-Na (College of Pharmacy, Chung Ang University ) , Lee Min-Won (College of Pharmacy, Chung Ang University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.2 ,pp. 177 - 179 , 2005 , 0253-6269 ,

    초록

    Nine known diarylheptanoids (1-9) isolated from the barks of Alnus japonica were evaluated for their inhibitory activities on nitric oxide (NO) and prostagrandin $E_2$ (COX-2) production in interferon- ${\gamma}$ (INF- ${\gamma}$ ) and lipopolysaccharide (LPS)-activated RAW 264.7 cells in vitro. The NO and COX-2 levels were moderately reduced by the addition of compounds (1-9). Among these compounds, compounds 6 and 8 inhibited NO production in a dose dependent manner with an $IC_{50}$ of 16.7 and $27.2\;{\mu}g/mL$ , respectively (positive control, L-NMMA; $22.8\;{\mu}g/mL$ ), and compounds 6, 7, 8, and 9 reduced the COX-2 level in a dose dependent manner with an $IC_{50}$ of 20.7, 25.7, 25.0, and $27.3\;{\mu}g/mL$ , respectively (positive control, indomethacin; $26.2\;{\mu}g/mL$ ). An analysis of the structural activity relationship among these diarylheptanoids suggests that the presence of a keto-enol group in the heptane moiety or a caffeoyl group in the aromatic ring were important for the efficacy on the inhibitory activities of NO and COX-2 production.

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  9. [국내논문]   In Vitro Inhibitory Effect of Triterpenoidal Saponins from Platycodi Radix on Pancreatic Lipase  

    Xu Bao Jun (Department of Food Science and Technology, College of Agriculture and Biotechnology, Chungnam National University, The Pharmaceutical Institute, Dalian University ) , Han Li Kun (Faculty of Environmental and Symbiotic Sciences, Prefectural University of Kumamoto ) , Zheng Yi Nan (College of Chinese Material Medicine, Jilin Agricultural University ) , Lee Jeong Hyun (Department of Food Science and Technology, College of Agriculture and Biotechnology, Chungnam National University ) , Sung Chang Keun (Department of Food Science and Technology, College of Agriculture and Biotechnology, Chungnam National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.2 ,pp. 180 - 185 , 2005 , 0253-6269 ,

    초록

    In the process of investigating anti-obesity effect of Platycodi Radix, we found that aqueous extract of Platycodi Radix might inhibit intestinal absorption of dietary fat by inhibiting pancreatic lipase (PL) activity. In order to clarify the anti-obesity mechanism of Platycodi Radix, activity-guided isolation was performed to find active components. The total saponin fraction of Platycodi Radix appeared to have a potent inhibitory activity against the hydrolysis of triolein emulsified with phosphatidycholine by pancreatic lipase in vitro. Based on these results, further purification of active components yielded 10 known triterpenoidal saponins, among these compounds, platycodin A, C, D, and deapioplatycodin D exhibited significant inhibitory effects on PL at the concentration of $500\;{\mu}g/mL$ with 3.3, 5.2, 34.8, and $11.67\%$ pancreatic lipase activity vs control, respectively. Platycodin D was found to inhibit the PL activity in a dose-dependent manner. Therefore, the anti-obesity effect of Platycodi Radix might be due to the inhibition of pancreatic lipase by its saponins.

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  10. [국내논문]   Anti-Estrogenic Activity of Lignans from Acanthopanax chiisanensis Root   피인용횟수: 3

    Lee Sanghyun (College of Pharmacy, Seoul National University ) , Yoo Hye Hyun (College of Pharmacy, Seoul National University ) , Piao Xiang Lan (College of Pharmacy, Seoul National University ) , Kim Ju Sun (Natural Products Research Institute, Seoul National University ) , Kang Sam Sik (Natural Products Research Institute, Seoul National University ) , Shin Kuk Hyun (Natural Products Research Institute, Seoul National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.2 ,pp. 186 - 189 , 2005 , 0253-6269 ,

    초록

    Anti-estrogenic activity of (-)-sesamin (1), helioxanthin (2), savinin (3), taiwanin C (4), and 3­(3,4-dimethoxybenzyl)-2-(3,4-methylenedioxybenzyl)butyrolactone (5) isolated from the root of Acanthopanax chiisanensis was tested using Ishikawa cells. Among them, compound 3 exhibited anti-estrogenic activity ( $IC_{50}\;=\;4.86\;{\mu}M$ ).

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